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Enhanced thermal stability of carbamazepine obtained by fast heating, hydration and re-crystallization from organic solvent solutions: A DSC and HPLC study
Thermochimica Acta ( IF 3.5 ) Pub Date : 2020-08-01 , DOI: 10.1016/j.tca.2020.178691
Agnieszka Dołęga , Anna Krupa , Piotr M. Zieliński

Abstract Although drugs are usually stored at room temperature, their thermal stability up to the melting point is often required for processing such as quenching or hot-melt extrusion. It especially concerns substances which have poor water solubility, as these techniques are used to either assess the glass forming ability or to prepare solid dispersions with the aim to enhance dissolution rate and bioavailability. Carbamazepine (CBZ), an antiepileptic drug, is an example of active pharmaceutical ingredient which shows both limited solubility in water and decomposition below melting point. This paper suggests and discusses different ways to enhance CBZ thermal stability, namely fast heating of the sample, hydration and re-crystallization from organic solvents (ethanol, acetone and dichloromethane). The presence of a model degradation product, i.e. iminostilbene is evaluated using differential scanning calorimetry and high-performance liquid chromatography. Obtained results show that all three proposed approaches are able to reduce the degree of CBZ thermal degradation, however none of them entirely stops the decomposition of CBZ in the vicinity of the melting point.

中文翻译:

通过从有机溶剂溶液中快速加热、水合和重结晶获得的卡马西平增强的热稳定性:DSC 和 HPLC 研究

摘要 虽然药物通常在室温下储存,但在淬火或热熔挤出等加工过程中,往往需要它们的热稳定性达到熔点。它特别关注水溶性差的物质,因为这些技术用于评估玻璃形成能力或制备固体分散体,目的是提高溶解速度和生物利用度。卡马西平 (CBZ) 是一种抗癫痫药,是一种活性药物成分,它在水中的溶解度有限,而且在熔点以下会分解。本文提出并讨论了提高 CBZ 热稳定性的不同方法,即样品的快速加热、水合和从有机溶剂(乙醇、丙酮和二氯甲烷)中重结晶。模型降解产物的存在,即 使用差示扫描量热法和高效液相色谱法评估亚氨基芪。获得的结果表明,所有三种提出的方​​法都能够降低 CBZ 热降解的程度,但是它们都没有完全阻止 CBZ 在熔点附近的分解。
更新日期:2020-08-01
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